网站主页>>>项目整合精选>>>项目整合精选>>>Clarithromycin, 6-O-Methylerythromycin A, Abbott-56268, A-56268, TE-031, Naxy, Klaricid XL, Biaxin XL, Klaricid, Clarith, Biaxin, Cyllind, Macladin, Veclam, Klacid

Clarithromycin, 6-O-Methylerythromycin A, Abbott-56268, A-56268, TE-031, Naxy, Klaricid XL, Biaxin XL, Klaricid, Clarith, Biaxin, Cyllind, Macladin, Veclam, Klacid

克拉霉素Chemical Name: 6-O-Methylerythromycin
CAS No. 81103-11-9
项目整合开发状态: Launched-1990
项目研究机构: Taisho (Originator), Sanofi-Aventis (Not Determined), Dainippon Pharmaceutical (Marketer), Abbott (Licensee), Guidotti (Licensee), Malesci (Licensee)
合成路线:The methylation of 2'-O,N-bis(benzyloxycarbonyl)-N-demethylerythromycin A (I) with methyl iodide and KOH or NaHI in DMSO-dimethoxyethane gives the 6-O-methyl derivative (II),which is deprotected by hydrogenation with H2 over Pd/C in ethanol acetic acid affording 6-O-methyl-N-demethylerythromycin A (III).Finally,this compound is methylated with formaldehyde under reductive conditions (H2-Pd/C) in ethanol/acetic acid.
📌 参考资料/链接:
参考文献标题:Novel erythromycin compounds
文献作者:Watanabe,Y.; Morimoto,S.; Omura,S.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:EP 0041355; US 4331803

📄 详细内容


合成路线:The methylation of 2'-O,N-bis(benzyloxycarbonyl)-N-demethylerythromycin A (I) with methyl iodide and KOH or NaHI in DMSO-dimethoxyethane gives the 6-O-methyl derivative (II),which is deprotected by hydrogenation with H2 over Pd/C in ethanol acetic acid affording 6-O-methyl-N-demethylerythromycin A (III).Finally,this compound is methylated with formaldehyde under reductive conditions (H2-Pd/C) in ethanol/acetic acid.

参考文献标题:Method for preparing 6-O-methyl-2'-O,N-bis(benzyloxycarbonyl)-N-dimethylerythromycin a
文献作者:Adachi,T.; Kikugawa,Y.; Morimoto,S.; Sota,K.; Takahashi,Y.; Watanabe,Y.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:EP 0147062


合成路线:The methylation of 2'-O,N-bis(benzyloxycarbonyl)-N-demethylerythromycin A (I) with methyl iodide and KOH or NaHI in DMSO-dimethoxyethane gives the 6-O-methyl derivative (II),which is deprotected by hydrogenation with H2 over Pd/C in ethanol acetic acid affording 6-O-methyl-N-demethylerythromycin A (III).Finally,this compound is methylated with formaldehyde under reductive conditions (H2-Pd/C) in ethanol/acetic acid.

参考文献标题:6-O-Methylerythromycin A
文献作者:Serradell,M.N.; Castar,R.M.; Castar,J.
参考来源:Drugs Fut 1987,12(10),952


合成路线:The methylation of 2'-O,N-bis(benzyloxycarbonyl)-N-demethylerythromycin A (I) with methyl iodide and KOH or NaHI in DMSO-dimethoxyethane gives the 6-O-methyl derivative (II),which is deprotected by hydrogenation with H2 over Pd/C in ethanol acetic acid affording 6-O-methyl-N-demethylerythromycin A (III).Finally,this compound is methylated with formaldehyde under reductive conditions (H2-Pd/C) in ethanol/acetic acid.
参考文献标题:Chemical modification of erythromycins.1.Synthesis and antibacterial activity of 6-O-methylerythromycins A
文献作者:Morimoto,S.; Takahashi,Y.; Watanabe,Y.; Omura,S.
参考来源:J Antibiot 1984,37(2),187-189


产品链接: CAS No. 81103-11-9››